The present invention relates to an antibacterial agent of the 1-.beta.-methyl-carbapenem class, in which the 2-position side-chain consists of a fluoren-9-on-3-yl group which is substituted by a (bis-quaternary ammonium)methyl moiety.
U.S. Pat. No. 5,034,384 issued on Jul. 23, 1991 generally discloses 2-(fluoren-9-on-2-yl)- and 2-(fluoren-9-on-3-yl)-carbapenems as having anti-MRSA/MRCNS activity. Likewise, EP Publication No. 0 472 306 A 1 which was published on Feb. 26, 1992 discloses said 2-(fluoren-9-on-2-yl)- and 2-(fluoren-9-on-3-yl)-carbapenems.
The 2-(fluoren-9-on-3-yl)-carbapenem of the present invention is characterized by an antibacterial spectrum which is largely focused on gram-positive microorganisms, especially methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS). Also, the present compound has safety and pharmacokinetic profiles which are superior to other compounds in the class.
There is an increasing need for agents which are effective against these pathogens (MRSA/MRCNS) and which are considered safe, i.e., relatively free from undesirable toxic side effects. The antibacterial compound of the present invention thus comprises an important contribution to therapy of these difficult to control pathogens.